A new series of compds., in which the 2-amino-4-methoxyphenyl ring of a phenstatin analog was replaced with 2- or 3-amino-benzoheterocycles, was synthesized and evaluated for antiproliferative activity and inhibition of colchicine binding. The lack of activity of 3',4'-dimethoxy- and 4'-methoxy-benzoyl derivs. indicates that the 3',4',5'-trimethoxybenzoyl moiety is crit. for the activity. Two compds. (I and II), displayed potent antiproliferative activity, with IC50 values ranging from 25 to 100 nM against a variety of cancer cell lines. Deriv. II was more active than CA-4 as an inhibitor of tubulin polymn. The results demonstrated that the antiproliferative activity was correlated with inhibition of tubulin polymn.
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles
ROMAGNOLI, Romeo;BARALDI, Pier Giovanni;IACONINOTO, Antonietta;PRETI, Delia;AGHAZADEH TABRIZI, Mojgan;FRUTTAROLO, Francesca;
2005
Abstract
A new series of compds., in which the 2-amino-4-methoxyphenyl ring of a phenstatin analog was replaced with 2- or 3-amino-benzoheterocycles, was synthesized and evaluated for antiproliferative activity and inhibition of colchicine binding. The lack of activity of 3',4'-dimethoxy- and 4'-methoxy-benzoyl derivs. indicates that the 3',4',5'-trimethoxybenzoyl moiety is crit. for the activity. Two compds. (I and II), displayed potent antiproliferative activity, with IC50 values ranging from 25 to 100 nM against a variety of cancer cell lines. Deriv. II was more active than CA-4 as an inhibitor of tubulin polymn. The results demonstrated that the antiproliferative activity was correlated with inhibition of tubulin polymn.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
